Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 45, Issue 2, Pages 588-597Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2009.10.047
Keywords
Phenstatin; Indole; Tubulin; Combretastatin; Cytotoxicity; Antitumour; Oxime; Hydrazone; Hydrazide; Acetylderivatives; 2,3,4-Trimethoxyphenyl
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Funding
- Junta de Castilla y Leon [SA 090A06, SA 067A09, SA 063A09]
- Spanish MEC [CTQ2004-00369/BQU]
- MICINN [SAF2008-04242, BFU2-02876]
- EU
- Fundacion Ramon Areces
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A new family of phenstatin analogues has been synthesized and assayed. This family simultaneously incorporates modifications of the A-ring (replacement of the 3,4,5-trimethoxyphenyl by the 2,3,4-trimethoxyphenyl arrangement), B-ring (N-alkyl-5-indolyl) and conversion of the Oxygen keto group into a substituted nitrogen (oximes, hydrazones, and their acetylderivatives). The conjunction of all this changes greatly diminishes the antimitotic and antiproliferative activities, but the maintenance of the keto bridge produces a potent analogue with the unusual 2,3,4-trimethoxyphenyl moiety. (C) 2009 Elsevier Masson SAS. All rights reserved.
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